Results 241 to 250 of about 71,002 (280)

Poly(ADP-Ribose) Polymerase Inhibitors

Current Medicinal Chemistry, 2003
Poly(ADP-ribose) polymerase-1 (PARP-1) is the principal member of the PARP enzyme family consisting of PARP-1 and several recently identified novel poly(ADP-ribosyl)ating enzymes. PARP-1 functions as a DNA damage sensor and signalling molecule. Upon binding to DNA breaks, activated PARP cleaves NAD(+) into nicotinamide and ADP-ribose and polymerizes ...
Garry J, Southan, Csaba, Szabó
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Current role of poly(ADP-ribose) polymerase inhibitors: which poly(ADP-ribose) polymerase inhibitor and when?

Current Opinion in Oncology, 2019
Purpose of review In the past few years, the advent of PARP inhibitors has been a revolution in the management of ovarian cancer. Patients harboring somatic or germ line BRCA1/2 mutations exhibit different clinical and treatment response behavior.
Hélène, Vanacker, Clémence, Romeo, Isabelle, Ray-Coquard   +2 more
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Natural Inhibitors of Poly(ADP-ribose) Polymerase-1

Molecular Neurobiology, 2012
Poly(ADP-ribose) polymerases (PARPs) are enzymes that catalyze the transfer of ADP-ribose units from β-nicotinamide adenine dinucleotide (NAD(+)) to acceptor proteins. PARP-1 is responsible for more than 90 % of protein poly-ADP-ribosylation in the brain and may play a role as a molecular switch for cell survival and death. The functional roles of PARP-
Marek, Banasik, Todd, Stedeford, Robert P, Strosznajder   +2 more
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Poly (ADP-ribose) Polymerase Inhibitors in Cancer Treatment

American Journal of Clinical Oncology, 2014
Recent research on inhibitors of poly (ADP-ribose) polymerase (PARP) has demonstrated their potential for improving cancer therapy. They inhibit protein poly (ADP-ribosyl)ation and thus affect numerous molecular and cellular functions, including DNA repair and cell survival, that are critical for such physiological and patho-physiological states as ...
Kathryn A, Mason, Uma, Raju, Thomas A, Buchholz, Li, Wang, Zvonimir L, Milas, Luka, Milas   +5 more
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Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase

Bioorganic and Medicinal Chemistry Letters, 2008
We have previously described poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a substituted benzyl-phthalazinone scaffold. As an alternative chemical template, a novel series of alkoxybenzamides were developed with restricted conformation through intramolecular hydrogen bond formation; the compounds exhibit low nM enzyme and cellular activity
Keith A, Menear, Claire, Adcock, Francisco Cuenca, Alonso, Kristel, Blackburn, Louise, Copsey, Jan, Drzewiecki, Alexandra, Fundo, Armelle, Le Gall, Sylvie, Gomez, Hashim, Javaid, Carlos Fenandez, Lence, Niall M B, Martin, Chris, Mydlowski, Graeme C M, Smith   +13 more
exaly   +3 more sources

The Therapeutic Potential of Poly(ADP-Ribose) Polymerase Inhibitors

Pharmacological Reviews, 2002
Poly(ADP-ribose) polymerase-1 (PARP-1) is a member of the PARP enzyme family consisting of PARP-1 and several recently identified novel poly(ADP-ribosylating) enzymes. PARP-1 is an abundant nuclear protein functioning as a DNA nick-sensor enzyme. Upon binding to DNA breaks, activated PARP cleaves NAD(+) into nicotinamide and ADP-ribose and polymerizes ...
László, Virág, Csaba, Szabó
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Poly(ADP-Ribose) Polymerase Inhibitor Combination Therapy

The Cancer Journal, 2021
Abstract The introduction of poly(ADP-ribose) polymerase (PARP) inhibitors has led to significant improvements in outcome for several cancer types, most notably high-grade serous ovarian cancer. However, in general, benefit is restricted to tumors characterized by either BRCA1/2 mutation or homologous recombination deficiency.
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Structural requirements for inhibitors of poly(ADP-ribose) Polymerase

Journal of Cancer Research and Clinical Oncology, 1990
The purpose of this study was to examine the structure/activity relationships of a series of substituted benzamides as poly(ADP-ribose) polymerase inhibitors. The experimental approach has involved the use of in vitro and in vivo assays in order to gather information either on the intrinsic activity of the benzamides or on the effect of various ...
SESTILI, PIERO, SPADONI, GILBERTO, BALSAMINI, CESARINO, SCOVASSI I, CATTABENI F, DURANTI E, CANTONI, ORAZIO, HIGGINS D, THOMSON C.   +8 more
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Novel poly(ADP-ribose) polymerase-1 inhibitors

Bioorganic & Medicinal Chemistry Letters, 2007
Synthesis and activity of a series of 3-aroyl-derived analogs of novel pyrrolocarbazole 1 as poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors are disclosed.
Derek, Dunn, Jean, Husten, Mark A, Ator, Sankar, Chatterjee   +3 more
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Some protease inhibitors are also inhibitors of poly(ADP-ribose) polymerase

Carcinogenesis, 1986
The low-molecular-weight peptide protease inhibitors, tosyl-lysine-chloromethyl ketone, antipain and leupeptin, inhibited poly(ADP-ribose) [poly(ADP-Rib)] polymerase in permeable cells. The concentrations required for 50% inhibition were 3.6, 5 and 29 mM, respectively. Two peptides without protease inhibitor activity, fibrinopeptide A and phenylalanine-
J E, Cleaver, M J, Banda, W, Troll, C, Borek   +3 more
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